4‐Aminoquinoline‐β‐Lactam Conjugates: Synthesis, Antimalarial, and Antitubercular Evaluation. (28th October 2013)

• Record Type: Journal Article
• Authors: Raj, Raghu; Biot, Christophe; Carrère‐Kremer, Séverine; Kremer, Laurent; Guérardel, Yann; Gut, Jiri; Rosenthal, Philip J.; Kumar, Vipan
• Is Part Of: Chemical biology & drug design. Volume 83:Number 2(2014:Feb.)
• Page Start: 191
• Page End: 197
• Publication Date: 2013-10-28
• Subjects: Drugs -- Design -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; 615.19005
• DOI: 10.1111/cbdd.12225
• Languages: English
• ISSNs: 1747-0277

Abstract

<abstract abstract-type="main" id="cbdd12225-abs-0001"> <title> <x xml:space="preserve">Abstract</x> </title> <p>A library of quinoline‐<italic>β</italic>‐lactam‐based hybrids was synthesized and tested for their antimalarial and antitubercular activities. The present antimalarial data showed the dependence of activity on the nature of linker, <italic>N</italic>‐1 substituent of the <italic>β</italic>‐lactam ring as well as the length of alkyl chain. Most of the compounds are not as efficient as chloroquine in inhibiting the culture growth of <italic>Plasmodium falciparum </italic>W2 strain. Nevertheless, the synthesized hybrids showed better antitubercular activities (up to five times) compared with cephalexin (up to three times) and ethionamide.</p> </abstract>